Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
185 words
A process for preparing a compound of the structure wherein R 1 is -S iR 3 R 4 R 5 R 2 is hydrogen, -SiR 3 R 4 R 5 or acyl; and R 3 , R 4 and R 5 are each independently alkyl of 1-8 carbon atoms, alkenyl of 1-8 carbon atoms, aralkyl of 7-10 carbon atoms, triphenylmethyl, or phenyl, providing that when more than one SiR 3 R 4 R 5 group is present they may be the same or different, which comprises silylating rapamycin using a silylating agent containing the group R 3 R 4 R 5 Si- to give a compound of structure I wherein R 1 is -SiR 3 R 4 R 5 and R 2 is hydrogen or -SiR 3 R 4 R 5 and if required acylating a product wherein R 2 is hydrogen to give a corresponding compound of structure I wherein R 2 is acyl, or if desired further silylating a product where R 2 is hydrogen to give a compound of formula I wherein R 2 is SiR 3 R 4 R 5 .
Claim 2
Dependent Claim
17 words
A process as claimed in Claim 1 in which R 2 in the compound prepared is hydrogen.
Claim 3
Dependent Claim
15 words
A process according to Claim 1 where R 2 in the compound prepared is acetyl.
Claim 4
Dependent Claim
30 words
A process as claimed in Claim 1 in which the silylating agent(s) is/are a silyl halide of formula R 3 R 4 R 5 Sihal where hal is a halogen.
Claim 5
Dependent Claim
21 words
A process as claimed in any one of Claims 1 to 3 wherein R 1 in the compound prepared is (1,1-dimethylethyl)dimethylsilyl.
Claim 6
Dependent Claim
24 words
A process as claimed in Claim 1 in which the product. is one of the following: rapamycin 42-O-[(1,1-dimethylethyl)dimethylsilyl ether, rapamycin 31,42-bis-O-[(1,1-dimethylethyl)dimethylsilyl]ether, or rapamycin 42-[O-[(1,1-dimethylethyl)dimethylsilyl]-ether-31-acetate.
Claim 7
Dependent Claim
28 words
A process for preparing a pharmaceutical composition which comprises bringing a compound of structure I as defined in Claim 1 to into association with a pharmaceutically acceptable carrier.
Claim 8
Dependent Claim
37 words
A process for preparing a 31-acylated rapamycin derivative which comprises hydrolysing a compound of structure I as defined in Claim 1 wherein R 1 is R 3 R 4 R 5 Si- and R 2 is acyl.
Claim 9
Dependent Claim
14 words
A process as claimed in Claim 8 in which the product is rapamycin 31-acetate.